Synthesis of [1-14C]1,2-cyclohexanedione bis(4-diethylenoxythiosemicarbazone) and preliminary biodistribution studies of this potential antitumor agent.

ABSTRACT

A new compound, [1-14C]1,2-cyclohexanedione-bis(4-diethylenoxythiosemicarbazone) was found to have significant antitumor activity (% T/C = 245) when tested against sarcoma-180 ascites tumor in mice and thus may be a potentially useful drug. The compound can be easily labeled with 14C by employing the straightforward synthetic procedures detailed in this article. Results of the synthesis and purification are presented. Preliminary biodistribution studies of the labeled compound in both normal and tumor bearing mice were performed. The compound, when administered i.p., is rapidly absorbed and localized into most tissues. Urinary and biliary excretion are its major routes of elimination. Based on these studies, continued evaluation is recommended.